Details for Patent: 5,439,666

Title:	Iodinated neuroprobe for mapping monoamine reuptake sites
Abstract:	An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein R=a C.sub.n H.sub.2n+1 group where n=0-6, an alkenyl group, a monofluoroalkyl group including .sup.n F where n=18 or 19, or a .sup.m C.sub.n H.sub.2n+1 group where n=1-6 and where m=11 or 14 for at least one .sup.m C; R'=a C.sub.n H.sub.2n+1 group where n=0-6, a p-iodophenylmethyl group, a p-iodophenylethyl group, a phenylmethyl group, or a phenylethyl group; X=an isotope of F, an isotope of Cl, an isotope of Br, an isotope of I, CH.sub.3, or Sn(R".sub.1 R".sub.2 R".sub.3); R".sub.1 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.2 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.3 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; and Y=H only if X is an isotope of I, or R' is a p-iodophenylmethyl group, or R' is a p-iodophenylethyl group, else Y=an isotope of I. Related analogs are also provided. Additionally, a precursor of a radiolabled neuroprobe and a kit for preparing the iodinated neuroprobe are provided.
Inventor(s):	Neumeyer; John L. (Wayland, MA), Milius; Richard A. (Boston, MA), Innis; Robert B. (Hamden, CT)
Assignee:	Research Biochemicals Limited Partnership (Natick, MA)
Filing Date:	Jan 24, 1994
Application Number:	08/185,689
Claims:	1. A kit for preparing a radiolabeled neuroprobe for mapping monoamine reuptake sites, the kit comprising: a precursor of the formula: ##STR4## wherein R=a monofluoroalkyl group; R'=a C.sub.n H.sub.2n+1 group where n=0-6; X=I or Sn(R".sub.1 R".sub.2 R".sub.3); R".sub.1 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.2 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.3 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; and Y=H. 2. The kit of claim 1, wherein said precursor is reacted in the presence of a radioisotope source. 3. The kit of claim 2 wherein the radioisotope source is a solution of a salt of a radioactive isotope of iodine, and said reaction takes place in the presence of an oxidizing agent. 4. A kit for preparing a radiolabeled neuroprobe for mapping monoamine reuptake sites, the kit comprising: a precursor of the formula: ##STR5## wherein R=a monofluoroalkyl group; R'=a C.sub.n H.sub.2n+1 group where n=0-6; X=I or Sn(R".sub.1 R".sub.2 R".sub.3); R".sub.1 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.2 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.3 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; and Y=H. 5. The kit of claim 4, wherein said precursor is reacted in the presence of a radioisotope source. 6. The kit of claim 5 wherein the radioisotope source is a solution of a salt of a radioactive isotope of iodine, and said reaction takes place in the presence of an oxidizing agent.